4.5 Article

Design, synthesis and biological evaluation of new thalidomide analogues as TNF-α and IL-6 production inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 3, Pages 1019-1022

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.12.031

Keywords

Thalidomide; TNF-alpha; IL-6; 1H-Imidazo[1,5-a]indole-dione; Dihydro-thiadiazolo[2,3-b]-isoquinolinone-dioxide; 1H-Pyrrolo-[2,3-b]pyridine

Funding

  1. Laboratory of Organic and Therapeutic Chemistry
  2. INCa (Institut National du Cancer
  3. MAb IMPACT network)

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Several thalidomide analogues were synthesized and compared to thalidomide and its more active analogue, lenalidomide, for their ability to inhibit the production of the pro-inflammatory cytokine tumour necrosis factor (TNF)-alpha and interleukin (IL)-6 by LPS-activated peripheral blood mononuclear cells (PBMCs). Among these compounds, two analogues containing sulfonyl group displayed interesting downregulation of TNF-alpha and IL-6 production. (C) 2010 Elsevier Ltd. All rights reserved.

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